Enzymes as Drug Targets (An Intro) - Medicinal Chemistry 1.11

Enzymes are essential for life, and dysregulated or mutated enzymes could lead to diseases. Enzyme-targeting drugs make up about 47% of marketed small-molecule drugs. Besides how important the catalytic activity of enzyme is, another reason that they are frequently targeted for therapeutics is that they are relatively easy to target or they are more druggable compared to other biomolecules.
Most small-molecule drugs that target enzymes are enzyme inhibitors. An enzyme inhibitor is a molecule that could bind to an enzyme and decreases its activity. Based on the inhibition mechanism, the inhibitors can be roughly divided into reversible and irreversible inhibitors. The reversible inhibitors can be further divided into competitive, noncompetitive uncompetitive and mixed inhibition, depending on the kinetics and inhibition mechanism.
Some enzyme-targeting drugs are enzyme activators that enhances the enzyme catalytic activity and sometimes the affinity of between the enzyme and the substrate.
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